99m Chemical structure and preparation method of tc-labeled rgd polypeptide trimer tumor imaging agent
A chemical structure and 99mtc technology, which is applied in the field of chemical structure and preparation of 99mTc-labeled RGD polypeptide trimer tumor imaging agents, can solve the problem of high radioactive background, high uptake value of non-target organs, and imaging of tumor sites that interfere with abdominal organs Effect and other issues
Active Publication Date: 2018-02-02
刘丽 +1
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[0007] Existing research results suggest that technetium-labeled RGD polypeptide dimer ( 99m Tc-3P-RGD 2 ) and technetium-labeled RGD galactose dimer ( 99m Tc-Galacto-RGD 2 ) imaging agent and integrin α in malignant tumors v beta 3 The expression has high affinity, and can be used as an economical agent for tumor diagnosis by SPECT or SPECT / CT imaging. However, the uptake of these two agents in non-target organs in animals is relatively high, especially the formation of higher radioactivity in abdominal organs. bottom, which can interfere with the imaging of tumor sites in abdominal organs
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[0016] RGD polypeptide trimer single-photon radiopharmaceutical preparation method:
[0017] 1. Materials and instruments: Purified chemical reagents were purchased from Sigma / Aldrich Company in the United States (St. Louis, MO). RGD polypeptide trimer (4P-RGD 3 ) is specially customized to Peptides International, Inc of the United States (Louisville, KY). HYNIC-Osu was formulated according to the method described in the literature. MALDI (matrix-assisted laser desorption ionization) mass spectrometry data were collected by Applied Biosystems Voyager DE PRO mass spectrometer (Framingham, MA). 99m TCO 4 - Obtained through drug sellers.
[0018] 2. HPLC (high performance liquid chromatography) analysis method:
[0019] 1. Method 1: the semi-preparative high-performance liquid chromatography (HPLC) analysis method used is equipped with the LabAlliance high-performance liquid chromatography analysis system and the Zorbax C18 semi-preparative chromatographic column (9.4nm ×2...
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The invention relates to a chemical structure and a preparation method of a tumor imaging agent, and in particular relates to a single photon emission computed tomography (SPECT) technetium (99mTc)-labeled RGD polypeptide trimer medicine, namely 99mTc-4P-RGD3. The tumor imaging medicine is combined with an integrin alphavbeta3 in a ligand mode so as to achieve an application of imaging a tumor part. The preparation method comprises the following implementing steps: linking HYNIC-Osu to 4P-RGD3 so as to obtain a ligand HYNIC-4P-RGD3, and chelating the HYNIC in the ligand with 99mTc so as to obtain the 99mTc-4P-RGD3 tumor imaging agent. A research on animal in-vivo distribution and a tumor imaging step proves that the tumor imaging agent is relatively high in tumor uptake and lower in background uptake to normal organs in a whole body, and the definition of tumor image of the whole body is improved; a drug metabolism experimental step shows that the 99mTc-4P-RGD3, after metabolized in an animal body, can be still discharged out of the body in a prototype mode. The technetium-labeled integrin alphavbeta3 tumor imaging agent (99mTc-4P-RGD3) prepared by the technical means disclosed by the invention can be used for solving a problem of high background uptake of other technetium-labeled RGD medicines in animal body, so that the technetium-labeled RGD medicine is more suitable for the assessment of tumors in whole body.
Description
【Technical field】 [0001] The present invention relates to the chemical structure and preparation method of a tumor imaging agent in single photon emission computed tomography (single photon emission computed tomography, SPECT), in particular to a technetium ( 99m Tc) labeled RGD (arginine-glycine-aspartic acid, Arg-Gly-Asp) polypeptide trimer drugs: 99m Tc-4P-RGD 3 , the drug can pass through the integrin (integrin) α in the tumor after intravenous injection v beta 3 Expressed, in a ligand manner, with integrin alpha v beta 3 The receptors combine with each other to achieve the purpose of imaging the tumor site. 【Background technique】 [0002] According to the [World Cancer Report] released by the World Health Organization (WHO), in recent years, the number of cancer patients in China has been 3.065 million, accounting for about 1 / 5 of the global incidence, and the number of cancer deaths is 2.205 million, accounting for about 20% of the global cancer deaths. 1 / 4, maki...
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IPC IPC(8): A61K51/08A61K103/10
Inventor 许百灵刘丽方纬
Owner 刘丽